3-beta-hydroxy-5-alpha-pregnan-20-one is a steroid in the pregnane family and a modulator of GABAA-receptor activity which is indicated for the treatment of sex/stress steroid induced disorders conditions (WO99/45931). 3-beta-hydroxy-5-alpha-pregnan-20-one is poorly soluble in many therapeutically acceptable solvents, which makes it difficult to administer the compound to a patient.
In animal studies, 3-beta-hydroxy-5-alpha-pregnan-20-one has been intravenously administered to rats in a formulation containing cyclodextrin (WO99/45931).
Grant et al (JPET 326:354-362, 2008) has administered 3-beta-hydroxy-5-alpha-pregnan-20-one to monkeys by using a formulation with hydroxypropyl β-cyclodextrin.
Formulations with cyclodextrins are not suitable for administration to human patients. One reason for this is, because 3-beta-hydroxy-5-alpha-pregnan-20-one is poorly soluble, the formulation results in a large therapeutic volume that can only be administered intravenously.
Since 3-beta-hydroxy-5-alpha-pregnan-20-one is poorly soluble in water there is still no pharmaceutically acceptable formulation for this compound.